Bioavailability of sugar-coated tablets of thiamine disulfide in humans. II. Correlation with bioavailability in beagle dogs.

Aoyagi, Nobuo; Ogata, Hiroyasu; Kaniwa, Nahoko; Koibuchi, Masanobu; Shibazaki, Toshio; Ejima, Akira; Mizobe, Masakazu; Kohno, Keiichi; Samejima, Masayoshi

doi:10.1248/cpb.34.292

Cited by 7 publications

(3 citation statements)

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“…TDS interacts with FA in l,2-dichloroethane1 whose dielectric constant (E = 10.65 at 20 "C) is similar to that of 1-octanol ( E = 10.34 at 20 "C), which is usually used to determine drug partition between skin and vehicle. The solubility of TDS in 1,2dichloroethane at 37 "C is 6.5 x lo-' M; the solubility increases to 1 In vitro studies of percutaneous absorption with furry animal skin do not provide information in agreement with in vitro studies with human skin because of the difference in the thickness of the stratum corneum and/or the abundance of appendageal pathways. But the mechanism by which a certain enhancer changes the permeability of organic solutes may be similar for skim from different species, although the magnitude of the morphological changes brought about by damage or disruption of the skin may be different for skins of different species.…”

Section: Resultsmentioning

confidence: 95%

In Vitro Percutaneous Absorption of Thiamine Disulfide from a Mixture of Propylene Glycol and Fatty Acid

Komata¹,

Inaoka²,

Kaneko³

et al. 1992

Journal of Pharmaceutical Sciences

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The in vitro percutaneous transport of thiamine disulfide (TDS), an oxidized dimer of thiamine, from propylene glycol through excised abdominal rat skin was studied. The application of saturated, long-chain fatty acids [stearic acid (18:0), myristic acid (14:0), and lauric acid (12:0)] as enhancers to the system was also studied. TDS permeated through rat skin from propylene glycol with a flux of 2.5 +/- 0.8 micrograms/cm2/min. The flux was enhanced 31 times by 12:0 and 1.4 times by 14:0 and was suppressed to 80% of its original value by 18:0. The absorption of TDS could not be explained by TDS permeating across a dialysis membrane, but the interaction between TDS and fatty acids may influence the system. The results show the possibility of developing a transdermal thiamine delivery system.

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Section: Resultsmentioning

confidence: 95%

In Vitro Percutaneous Absorption of Thiamine Disulfide from a Mixture of Propylene Glycol and Fatty Acid

Komata¹,

Inaoka²,

Kaneko³

et al. 1992

Journal of Pharmaceutical Sciences

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“…The data indicated that dogs with low gastric pH had significantly greater absorption of thiamine. Gastric pH ranged from approximately 3-6 and absorption (as measured by area under the plasma concentration vs time curve) varied from ∼5-50 hr-ng/ml (3).…”

Section: Gastrointestinalmentioning

confidence: 99%

Issues Related to the Use of Canines in Toxicologic Pathology—Issues With Pharmacokinetics and Metabolism

Tibbitts

2003

Toxicol Pathol

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The dog is a commonly used animal model by virtue of its size, well-characterized physiology, and ease of handling. For these reasons and others, dogs are also useful in pharmacokinetic and metabolism studies during the development of both human and veterinary pharmaceutical products. In comparison with humans, or with other animals, dogs have some unique physiologic attributes that can affect the disposition of drugs. Species differences in gastrointestinal physiology, metabolism, renal function, and protein binding can affect the correlation of the pharmacokinetics and toxicology of dogs with those of other species. With the use of relevant examples, this article will provide an introduction to characteristics of dog physiology and their impact on pharmacokinetics, metabolism, drug disposition, toxicity, and dose selection.

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“…Since the beagle dog is a species with similar metabolic activity to humans, the prediction of pharmacokinetics in humans may be more accurate [ 25 ]. In many references, it was found that the bioavailability relation between beagle dogs and humans is very high [ 26 , 27 ]. However, there is a disadvantage in that the difference of intestinal environment between beagle dogs and humans.…”

Section: Introductionmentioning

confidence: 99%

Novel Esomeprazole Magnesium-Loaded Dual-Release Mini-Tablet Polycap: Formulation, Optimization, Characterization, and In Vivo Evaluation in Beagle Dogs

Kwon

Kang

et al. 2022

Pharmaceutics

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Esomeprazole magnesium (EMP) is a proton pump inhibitor (PPI) that reduces acid secretion. EMP has a short plasma half-life (approximately 1.3 h); hence, nocturnal acid breakthrough (NAB) frequently occurs, disturbing the patient’s nighttime comfort and sleep. We aimed to develop a novel esomeprazole magnesium-loaded dual-release mini-tablet polycap (DR polycap) with a prolonged onset time and improved bioavailability to prevent NAB. The formulation of the EPM mini-tablet core resulted in rapid drug release. The core was coated with an inner coating and an Eudragit® L30D-55 aqueous dispersion coating to prepare the first-release mini-tablet. In addition, the core was coated with an inner coating and an aqueous dispersion of Eudragit® S100 and Eudragit® L100 coating to prepare the second-release mini-tablet. Each mini-tablet type was characterized using an in vitro dissolution test and microscopic examination. After testing, 10 of each mini-tablets were placed together in hard capsules to form DR polycaps. The combination of mini-tablets was optimized via in vitro release testing and in vivo pharmacokinetic studies. The AUC0–24h of the DR polycap was similar to that of a comparable commercial product (Nexium®); Cmax was lower by approximately 50%, and Tmax was extended by approximately 1.7-fold. In conclusion, DR polycap is an alternative to commercial products with improved NAB and dosing compliance because of its dual-release characteristics.

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Bioavailability of sugar-coated tablets of thiamine disulfide in humans. II. Correlation with bioavailability in beagle dogs.

Cited by 7 publications

References 0 publications

In Vitro Percutaneous Absorption of Thiamine Disulfide from a Mixture of Propylene Glycol and Fatty Acid

In Vitro Percutaneous Absorption of Thiamine Disulfide from a Mixture of Propylene Glycol and Fatty Acid

Issues Related to the Use of Canines in Toxicologic Pathology—Issues With Pharmacokinetics and Metabolism

Novel Esomeprazole Magnesium-Loaded Dual-Release Mini-Tablet Polycap: Formulation, Optimization, Characterization, and In Vivo Evaluation in Beagle Dogs

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